Stem definition | Drug id | CAS RN |
---|---|---|
Hepatitis Virus C (HVC) protease inhibitors | 4812 | 923604-59-5 |
Dose | Unit | Route |
---|---|---|
0.15 | g | O |
Property | Value | Reference |
---|---|---|
BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Hosey CM, Chan R, Benet LZ |
Date | Agency | Company | Orphan |
---|---|---|---|
May 14, 2014 | EMA | ||
Nov. 22, 2013 | FDA | JANSSEN PRODS |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Platelet count decreased | 773.97 | 36.36 | 301 | 4456 | 106082 | 56181228 |
Anaemia | 573.80 | 36.36 | 325 | 4432 | 267186 | 56020124 |
White blood cell count decreased | 464.65 | 36.36 | 221 | 4536 | 125769 | 56161541 |
Blood bilirubin increased | 388.10 | 36.36 | 134 | 4623 | 33220 | 56254090 |
Hepatitis C | 290.98 | 36.36 | 72 | 4685 | 5514 | 56281796 |
Neutrophil count decreased | 277.54 | 36.36 | 117 | 4640 | 49705 | 56237605 |
Haemoglobin decreased | 217.43 | 36.36 | 137 | 4620 | 134000 | 56153310 |
Hyperbilirubinaemia | 166.27 | 36.36 | 53 | 4704 | 10182 | 56277128 |
Haemolytic anaemia | 148.49 | 36.36 | 48 | 4709 | 9637 | 56277673 |
Hepatocellular carcinoma | 105.47 | 36.36 | 27 | 4730 | 2362 | 56284948 |
Pruritus | 101.79 | 36.36 | 129 | 4628 | 316494 | 55970816 |
Off label use | 94.57 | 36.36 | 168 | 4589 | 556012 | 55731298 |
Pyrexia | 91.90 | 36.36 | 142 | 4615 | 418631 | 55868679 |
Photosensitivity reaction | 85.86 | 36.36 | 35 | 4722 | 13558 | 56273752 |
Remission not achieved | 51.97 | 36.36 | 9 | 4748 | 113 | 56287197 |
Decreased appetite | 45.94 | 36.36 | 73 | 4684 | 219158 | 56068152 |
Hepatic failure | 43.74 | 36.36 | 30 | 4727 | 33456 | 56253854 |
Hepatic function abnormal | 42.88 | 36.36 | 30 | 4727 | 34528 | 56252782 |
Jaundice | 41.79 | 36.36 | 27 | 4730 | 27267 | 56260043 |
Hepatic encephalopathy | 40.82 | 36.36 | 19 | 4738 | 10091 | 56277219 |
Sunburn | 40.44 | 36.36 | 13 | 4744 | 2555 | 56284755 |
Hepatitis C RNA increased | 37.55 | 36.36 | 7 | 4750 | 136 | 56287174 |
Pain | 36.90 | 36.36 | 6 | 4751 | 663178 | 55624132 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Hepatitis C | 769.03 | 29.92 | 207 | 5476 | 10423 | 31681238 |
Platelet count decreased | 542.28 | 29.92 | 300 | 5383 | 110135 | 31581526 |
White blood cell count decreased | 391.37 | 29.92 | 224 | 5459 | 87174 | 31604487 |
Blood bilirubin increased | 352.96 | 29.92 | 156 | 5527 | 34980 | 31656681 |
Anaemia | 306.54 | 29.92 | 273 | 5410 | 213249 | 31478412 |
Hepatocellular carcinoma | 240.55 | 29.92 | 81 | 5602 | 8675 | 31682986 |
Off label use | 193.76 | 29.92 | 271 | 5412 | 347003 | 31344658 |
Hyperbilirubinaemia | 170.95 | 29.92 | 74 | 5609 | 15676 | 31675985 |
Haemoglobin decreased | 144.73 | 29.92 | 136 | 5547 | 112539 | 31579122 |
Neutrophil count decreased | 142.91 | 29.92 | 94 | 5589 | 46300 | 31645361 |
Photosensitivity reaction | 139.30 | 29.92 | 56 | 5627 | 9848 | 31681813 |
Drug ineffective | 90.62 | 29.92 | 210 | 5473 | 395363 | 31296298 |
Jaundice | 73.38 | 29.92 | 53 | 5630 | 30234 | 31661427 |
Remission not achieved | 71.07 | 29.92 | 13 | 5670 | 100 | 31691561 |
Pruritus | 67.92 | 29.92 | 97 | 5586 | 125070 | 31566591 |
Haemolytic anaemia | 59.83 | 29.92 | 31 | 5652 | 9765 | 31681896 |
Sunburn | 51.50 | 29.92 | 17 | 5666 | 1703 | 31689958 |
Treatment failure | 47.89 | 29.92 | 47 | 5636 | 40745 | 31650916 |
Hepatic failure | 46.68 | 29.92 | 42 | 5641 | 32660 | 31659001 |
Genotype drug resistance test positive | 45.88 | 29.92 | 14 | 5669 | 1087 | 31690574 |
Pyrexia | 44.43 | 29.92 | 137 | 5546 | 303703 | 31387958 |
Viral load increased | 43.74 | 29.92 | 16 | 5667 | 2173 | 31689488 |
Hepatitis C RNA increased | 42.86 | 29.92 | 10 | 5673 | 274 | 31691387 |
Hepatic encephalopathy | 42.71 | 29.92 | 28 | 5655 | 13643 | 31678018 |
Ascites | 42.19 | 29.92 | 44 | 5639 | 40969 | 31650692 |
Thought blocking | 38.68 | 29.92 | 8 | 5675 | 123 | 31691538 |
Bilirubin conjugated increased | 38.13 | 29.92 | 16 | 5667 | 3125 | 31688536 |
Rash | 34.27 | 29.92 | 96 | 5587 | 201390 | 31490271 |
Choroiditis | 33.13 | 29.92 | 11 | 5672 | 1121 | 31690540 |
Hyperuricaemia | 32.84 | 29.92 | 19 | 5664 | 7419 | 31684242 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Platelet count decreased | 1363.06 | 30.23 | 600 | 9114 | 177622 | 70741108 |
Hepatitis C | 940.26 | 30.23 | 239 | 9475 | 12568 | 70906162 |
White blood cell count decreased | 897.17 | 30.23 | 444 | 9270 | 169697 | 70749033 |
Anaemia | 855.84 | 30.23 | 581 | 9133 | 402842 | 70515888 |
Blood bilirubin increased | 692.15 | 30.23 | 272 | 9442 | 59629 | 70859101 |
Neutrophil count decreased | 414.53 | 30.23 | 210 | 9504 | 83346 | 70835384 |
Haemoglobin decreased | 365.24 | 30.23 | 267 | 9447 | 204892 | 70713838 |
Hepatocellular carcinoma | 346.11 | 30.23 | 104 | 9610 | 10104 | 70908626 |
Hyperbilirubinaemia | 315.56 | 30.23 | 118 | 9596 | 22450 | 70896280 |
Haemolytic anaemia | 202.99 | 30.23 | 79 | 9635 | 16715 | 70902015 |
Pruritus | 153.12 | 30.23 | 211 | 9503 | 345349 | 70573381 |
Photosensitivity reaction | 139.49 | 30.23 | 63 | 9651 | 19277 | 70899453 |
Pyrexia | 136.64 | 30.23 | 273 | 9441 | 606679 | 70312051 |
Jaundice | 109.07 | 30.23 | 74 | 9640 | 50034 | 70868696 |
Remission not achieved | 104.54 | 30.23 | 21 | 9693 | 369 | 70918361 |
Off label use | 89.84 | 30.23 | 263 | 9451 | 742797 | 70175933 |
Hepatic failure | 84.38 | 30.23 | 67 | 9647 | 57558 | 70861172 |
Hepatic encephalopathy | 66.32 | 30.23 | 40 | 9674 | 22078 | 70896652 |
Hepatitis C RNA increased | 63.47 | 30.23 | 14 | 9700 | 392 | 70918338 |
Bilirubin conjugated increased | 61.25 | 30.23 | 24 | 9690 | 5157 | 70913573 |
Rash | 59.80 | 30.23 | 179 | 9535 | 510383 | 70408347 |
Pain | 59.43 | 30.23 | 8 | 9706 | 628808 | 70289922 |
Ascites | 56.01 | 30.23 | 57 | 9657 | 67490 | 70851240 |
Hyperuricaemia | 55.45 | 30.23 | 28 | 9686 | 10938 | 70907792 |
Sunburn | 54.73 | 30.23 | 20 | 9694 | 3551 | 70915179 |
Decreased appetite | 53.10 | 30.23 | 124 | 9590 | 304656 | 70614074 |
Insomnia | 47.45 | 30.23 | 97 | 9617 | 217709 | 70701021 |
Malaise | 47.08 | 30.23 | 148 | 9566 | 432784 | 70485946 |
Hepatorenal syndrome | 45.61 | 30.23 | 18 | 9696 | 3939 | 70914791 |
Aspartate aminotransferase increased | 45.01 | 30.23 | 70 | 9644 | 126908 | 70791822 |
Hepatic function abnormal | 41.76 | 30.23 | 49 | 9665 | 67947 | 70850783 |
Red blood cell count decreased | 41.39 | 30.23 | 43 | 9671 | 52118 | 70866612 |
Hepatic cirrhosis | 41.29 | 30.23 | 34 | 9680 | 30697 | 70888033 |
Thought blocking | 37.53 | 30.23 | 8 | 9706 | 190 | 70918540 |
Viral load increased | 37.48 | 30.23 | 14 | 9700 | 2642 | 70916088 |
Choroiditis | 34.54 | 30.23 | 11 | 9703 | 1290 | 70917440 |
Liver disorder | 33.93 | 30.23 | 42 | 9672 | 61526 | 70857204 |
Alanine aminotransferase increased | 32.46 | 30.23 | 66 | 9648 | 147414 | 70771316 |
Injection site dermatitis | 31.64 | 30.23 | 5 | 9709 | 19 | 70918711 |
Incorrect product administration duration | 30.96 | 30.23 | 19 | 9695 | 10805 | 70907925 |
None
Source | Code | Description |
---|---|---|
ATC | J05AP05 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Antivirals for treatment of HCV infections |
MeSH PA | D000890 | Anti-Infective Agents |
MeSH PA | D000998 | Antiviral Agents |
MeSH PA | D004791 | Enzyme Inhibitors |
MeSH PA | D011480 | Protease Inhibitors |
FDA MoA | N0000182138 | Cytochrome P450 1A2 Inhibitors |
FDA MoA | N0000182141 | Cytochrome P450 3A4 Inhibitors |
FDA MoA | N0000182638 | HCV NS3/4A Protease Inhibitors |
FDA EPC | N0000182639 | Hepatitis C Virus NS3/4A Protease Inhibitor |
FDA MoA | N0000185503 | P-Glycoprotein Inhibitors |
FDA MoA | N0000190107 | Organic Anion Transporting Polypeptide 1B1 Inhibitors |
FDA MoA | N0000190108 | Organic Anion Transporting Polypeptide 1B3 Inhibitors |
FDA MoA | N0000190113 | Breast Cancer Resistance Protein Inhibitors |
FDA MoA | N0000193845 | Bile Salt Export Pump Inhibitors |
FDA MoA | N0000193960 | Multidrug Resistance-Associated Protein 2 Inhibitors |
FDA MoA | N0000193965 | Sodium Taurocholate Co-transporting Polypeptide Inhibitors |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Chronic hepatitis C | indication | 128302006 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 4.35 | acidic |
pKa2 | 6.66 | Basic |
pKa3 | 3.5 | Basic |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
---|---|---|---|---|---|---|---|---|---|---|
EQ 150MG BASE | OLYSIO | JANSSEN PRODS | N205123 | Nov. 22, 2013 | DISCN | CAPSULE | ORAL | 8349869 | July 28, 2026 | METHOD OF TREATING HEPATITIS C |
EQ 150MG BASE | OLYSIO | JANSSEN PRODS | N205123 | Nov. 22, 2013 | DISCN | CAPSULE | ORAL | 8741926 | July 28, 2026 | METHOD OF TREATING HEPATITIS C |
EQ 150MG BASE | OLYSIO | JANSSEN PRODS | N205123 | Nov. 22, 2013 | DISCN | CAPSULE | ORAL | 8754106 | July 28, 2026 | METHOD OF TREATING HEPATITIS C |
EQ 150MG BASE | OLYSIO | JANSSEN PRODS | N205123 | Nov. 22, 2013 | DISCN | CAPSULE | ORAL | 9040562 | July 28, 2026 | METHOD OF TREATING HEPATITIS C |
EQ 150MG BASE | OLYSIO | JANSSEN PRODS | N205123 | Nov. 22, 2013 | DISCN | CAPSULE | ORAL | 9353103 | July 28, 2026 | METHOD OF TREATING HEPATITIS C |
EQ 150MG BASE | OLYSIO | JANSSEN PRODS | N205123 | Nov. 22, 2013 | DISCN | CAPSULE | ORAL | 9623022 | July 28, 2026 | METHOD OF TREATING HEPATITIS C |
EQ 150MG BASE | OLYSIO | JANSSEN PRODS | N205123 | Nov. 22, 2013 | DISCN | CAPSULE | ORAL | 9856265 | July 28, 2026 | METHOD OF TREATING HEPATITIS C |
EQ 150MG BASE | OLYSIO | JANSSEN PRODS | N205123 | Nov. 22, 2013 | DISCN | CAPSULE | ORAL | 8148399 | Sept. 5, 2029 | METHOD OF TREATING HEPATITIS C |
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Cathepsin S | Enzyme | IC50 | 6.10 | CHEMBL | |||||
Hepatitis C virus serine protease, NS3/NS4A | Enzyme | INHIBITOR | Ki | 9.30 | CHEMBL | CHEMBL | |||
Genome polyprotein | Polyprotein | INHIBITOR | Ki | 9.44 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
Polyprotein | Polyprotein | INHIBITOR | Ki | 9.44 | IUPHAR | ||||
Nonstructural protein NS3-4A | Unclassified | Ki | 9.44 | CHEMBL | |||||
Genome polyprotein | Unclassified | Ki | 9.30 | CHEMBL |
ID | Source |
---|---|
D10081 | KEGG_DRUG |
4032900 | VANDF |
CHEBI:134743 | CHEBI |
30B | PDB_CHEM_ID |
CHEMBL501849 | ChEMBL_ID |
7367 | IUPHAR_LIGAND_ID |
9432 | INN_ID |
1241946-89-3 | SECONDARY_CAS_RN |
DB06290 | DRUGBANK_ID |
9WS5RD66HZ | UNII |
1482790 | RXNORM |
207569 | MMSL |
29896 | MMSL |
d08182 | MMSL |
015309 | NDDF |
015310 | NDDF |
708823009 | SNOMEDCT_US |
714167009 | SNOMEDCT_US |
C2605855 | UMLSCUI |
D000069616 | MESH_DESCRIPTOR_UI |
CHEMBL3137358 | ChEMBL_ID |
24873435 | PUBCHEM_CID |
None